【摘要】 雷公藤二萜内酯类化合物在结构上有一定的相似性:它们均含有3个六元环、1个五元内酯环和1～3个二元氧环,并且具有多种生物活性。本文选择了7个具有代表性的雷公藤二萜内酯化合物并通过X衍射分析获得其三维结构数据,以已有的药理实验数据为基础,对其精细立体结构变化和生物活性关系进行了探讨。研究结果表明:雷公藤萜内酯类化合物中的A、B、C三个六元环是其活性骨架的几何依托;18位上的羰基和7～8位上的三元氧环是其活性的可能结合部位;而该类化合物的活性部位则集中在C环的取代位置上;D环不是该类化合物具有生物活性的必需骨架部分。更多还原

【Abstract】 Tmperygium wnlfordu Hook. f diterpcne lactone compounds have similarity in structure. They all have three six-membered rings, one five-membered lactone rings, 1~ 3 epoxy three membered rings,and have many different biological activities. In our study,seven representative Tmperygium wil-fordu Hook, f diterpene lactone compounds were chosen for getting three-dimensional structural data by X-ray diffraction analysis,and the relations between fine stereo-structural changes and biological activities were approached based on known data from pharmacodynamic experiment. The result shows that six-membered ring A,B,C are the backings of activity;carbonyl group on position C18 and epoxy three-membered ring on position C7~C8 are the connecting parts;the activities of these compounds are accumulated on substitution positions of C ring;D ring is not a necessary backing part which has biological activity in these compounds.更多还原